CGP 20712 dihydrochloride

Catalog No. Size PriceQuantity
M22251-C Contact for quotation $100Unavailable


CGP 20712 dihydrochloride is a potent and selective antagonist of β1-adrenoceptor with IC50 value of 0.7 nM . β1-adrenoceptor is a G-protein coupled receptor and mediates uncoupling protein-1 (UCP1) gene expression induced by norepinephrine (NE) . CGP 20712 dihydrochloride is a potent and selective β1-adrenoceptor antagonist. In neocortical membranes, CGP 20712 A exhibited affinity for β1-adrenoceptor and β2-adrenoceptor with IC50 values of 0.7 and 6700 nM, respectively . In brown adipocytes, CGP-20712A significantly inhibited UCP1 gene expression induced by NE. However, CGP-20712A had no effect on lipolysis. These results suggested that β1-adrenoceptor mediated UCP1 gene expression . In ventricular membranes from rats, CGP 20712A (300 nM) completely occupied its high-affinity binding sites. In ventricular myocytes isolated from rats, CGP 20712A (10, 100, 1000 nM) didn’t cause the activation of adenylate cyclase mediated by β2-adrenoceptors, which suggested that β2-adrenoceptors were not present on rat ventricular myocytes . In adult rat cardiac myocytes, CGP 20712A inhibited β1-AR-stimulated apoptosis, which was mediated by a cAMP-dependent mechanism .

Product information

CAS Number: 1216905-73-5

Molecular Weight: 567.39

Formula: C23H27Cl2F3N4O5

Chemical Name: 2-hydroxy-5-{2-[(2-hydroxy-3-{4-[1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl]phenoxy}propyl)amino]ethoxy}benzene-1-carboximidic acid dihydrochloride

Smiles: Cl.Cl.CN1C=C(N=C1C1C=CC(=CC=1)OCC(O)CNCCOC1C=CC(O)=C(C=1)C(=N)O)C(F)(F)F


InChi: InChI=1S/C23H25F3N4O5.2ClH/c1-30-12-20(23(24,25)26)29-22(30)14-2-4-16(5-3-14)35-13-15(31)11-28-8-9-34-17-6-7-19(32)18(10-17)21(27)33;;/h2-7,10,12,15,28,31-32H,8-9,11,13H2,1H3,(H2,27,33);2*1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.

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